[关键词]
[摘要]
目的 研究白术的主要活性成分白术内酯I、Ⅱ、Ⅲ体内外抗轮状病毒(RV)的作用。方法 以Caco-2细胞建立体外研究模型,采用细胞病变效应(CPE)法并结合MTT染色法,测定白术内酯I、Ⅱ、Ⅲ对细胞的毒性以及对RV生物合成、吸附的抑制作用,对RV的直接灭活作用,以利巴韦林为阳性对照药。结合半数有效浓度(EC50)和半数细胞毒性浓度(TC50)得出治疗指数(TI)值,并且以其作为评价指标。制备RV感染的乳鼠腹泻模型进行体内研究,观察乳鼠体征表现,根据腹泻分数以及体质量增长情况初步判断白术内酯Ⅲ的体内抗RV作用。结果 在体外研究中发现白术内酯Ⅲ具有直接灭活RV的作用,TI值为8;体内研究中白术内酯Ⅲ中剂量组抗RV效果最佳。结论 白术的主要活性成分白术内酯Ⅲ在体内外均具有一定的抗RV作用;白术内酯Ⅲ主要通过体外直接灭活RV而发挥作用。
[Key word]
[Abstract]
Objective To study the effects of atractylodes I, Ⅱ, and Ⅲ against rotavirus in vitro and in vivo.Methods An in vitro study model was established using Caco-2 cells. The cytopathic effect (CPE) and MTT staining were used to determine the toxicity of atractylenolide I, Ⅱ, and Ⅲ to cells for the inhibition of rotavirus biosynthesis, direct inactivation of rotavirus, and antiviral adsorption, with ribavirin as a positive drug. With half of the therapeutic concentration (EC50) and half of the cytotoxic concentration (TC50), the treatment index TI value was obtained and used as the evaluation index. An RV-infected model of suckling diarrhea was established in vivo to observe the signs and symptoms of the suckling mice, and the in vivo anti-rotavirus effect was preliminarily determined according to the diarrhea score and the weight gain.Results In vitro studies found that atractylenolide Ⅲ had the direct inactivation effect on rotavirus with TI value of 8; atractylodes Ⅲ medium-dose group has the best anti-rotavirus effect in vivo.Conclusion Atractylodes Ⅲ, the main active component of Atractylodes macrocephala, has significant anti-rotavirus effect in vitro and in vivo; Atractylenolide Ⅲ mainly works by directly inactivating rotavirus in vitro.
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[基金项目]
国家自然科学基金面上项目(81473401);广东省科技计划项目重大专项(2013A022100039);东莞市社会发展重点项目(东科[2018]167号,编号20185071521658)